963
Views
25
CrossRef citations to date
0
Altmetric
Reviews

c-FMS inhibitors: a patent review

, BSc (Hons) PhD & , BSc (Hons) PhD
Pages 147-165 | Published online: 05 Jan 2011

Bibliography

  • Fredriksson L, Li H, Eriksson U. The PDGF family: four gene products form five dimeric isoforms. Cytokine Growth Factor Rev 2004;15(4):197-204
  • Williams DE, Eisenman J, Baird A, Identification of a ligand for the c-kit proto-oncogene. Cell 1990;63(1):167-74
  • Lyman SD, James L, Vanden Bos T, Molecular cloning of a ligand for the flt3/flk-2 tyrosine kinase receptor: a proliferative factor for primitive hematopoietic cells. Cell 1993;75(6):1157-67
  • Sherr CJ, Rettenmier CW, Sacca R, The c-fms proto-oncogene product is related to the receptor for the mononuclear phagocyte growth factor, CSF-1. Cell 1985;41(3):665-76
  • Lin H, Lee E, Hestir K, Discovery of a cytokine and its receptor by functional screening of the extracellular proteome. Science 2008;320(5877):807-11
  • Hamilton JA. CSF-1 signal transduction. J Leukoc Biol 1997;62(2):145-55
  • Walter M, Lucet IS, Patel O, The 2.7 A crystal structure of the autoinhibited human c-Fms kinase domain. J Mol Biol 2007;367(3):839-47
  • Schubert C, Schalk-Hihi C, Struble GT, Crystal structure of the tyrosine kinase domain of colony-stimulating factor-1 receptor (cFMS) in complex with two inhibitors. J Biol Chem 2007;282(6):4094-101
  • Huang H, Hutta DA, Rinker JM, Pyrido[2,3-d]pyrimidin-5-ones: a novel class of anti-inflammatory macrophage colony-stimulating factor-1 receptor inhibitors. J Med Chem 2009;52(4):1081-99
  • Meyers MJ, Pelc M, Kamtekar S, Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode. Bioorg Med Chem Lett 2010;20(5):1543-7
  • Chitu V, Stanley ER. Colony-stimulating factor-1 in immunity and inflammation. Curr Opin Immunol 2006;18(1):39-48
  • Douglass TG, Driggers L, Zhang JG, Macrophage colony stimulating factor: not just for macrophages anymore! A gateway into complex biologies. Int Immunopharmacol 2008;8(10):1354-76
  • Takashima A, Edelbaum D, Kitajima T, Colony-stimulating factor-1 secreted by fibroblasts promotes the growth of dendritic cell lines (XS series) derived from murine epidermis. J Immunol 1995;154(10):5128-35
  • Ginhoux F, Tacke F, Angeli V, Langerhans cells arise from monocytes in vivo. Nat Immunol 2006;7(3):265-73
  • Fancke B, Suter M, Hochrein H, O'Keeffe M. M-CSF: a novel plasmacytoid and conventional dendritic cell poietin. Blood 2008;111(1):150-9
  • Pandit J, Bohm A, Jancarik J, Three-dimensional structure of dimeric human recombinant macrophage colony-stimulating factor. Science 1992;258(5086):1358-62
  • Mackaness GB. The immunological basis of acquired cellular resistance. J Exp Med 1964;120:105-20
  • Porcheray F, Viaud S, Rimaniol AC, Macrophage activation switching: an asset for the resolution of inflammation. Clin Exp Immunol 2005;142(3):481-9
  • Mantovani A, Sozzani S, Locati M, Macrophage polarization: tumor-associated macrophages as a paradigm for polarized M2 mononuclear phagocytes. Trends Immunol 2002;23(11):549-55
  • Ginhoux F, Tacke F, Angeli V, Langerhans cells arise from monocytes in vivo. Nat Immunol 2006;7(3):265-73
  • Takashima A, Kitajima T. T cell-mediated terminal maturation of dendritic cells, a critical transition into fully potent antigen presenting cells. Pathol Biol (Paris) 1998;46(1):53-60
  • Nakajima K, Kohsaka S. Microglia: activation and their significance in the central nervous system. J Biochem 2001;130(2):169-75
  • Imai Y, Kohsaka S. Intracellular signaling in M-CSF-induced microglia activation: role of Iba1. Glia 2002;40(2):164-74
  • Kondo Y, Lemere C, Seabrook T. Osteopetrotic (op/op) mice have reduced microglia, no Abeta deposition, and no changes in dopaminergic neurons. J Neuroinflamm 2007;4(1):31
  • Nijweide PJ, Burger EH, Feyen JH. Cells of bone: proliferation, differentiation, and hormonal regulation. Physiol Rev 1986;66(4):855-86
  • Lacey DL, Timms E, Tan HL, Osteoprotegerin ligand is a cytokine that regulates osteoclast differentiation and activation. Cell 1998;93(2):165-76
  • Teitelbaum SL. Osteoclasts: what do they do and how do they do it? Am J Pathol 2007;170(2):427-35
  • Yasuda H, Shima N, Nakagawa N, Osteoclast differentiation factor is a ligand for osteoprotegerin/osteoclastogenesis-inhibitory factor and is identical to TRANCE/RANKL. Proc Natl Acad Sci USA 1998;95(7):3597-602
  • Wiktor-Jedrzejczak W, Bartocci A, Ferrante AW, Total absence of colony-stimulating factor 1 in the macrophage-deficient osteopetrotic (op/op) mouse. Proc Natl Acad Sci USA 1990;87(12):4828-32
  • Yoshida H, Hayashi S, Kunisada T, The murine mutation osteopetrosis is in the coding region of the macrophage colony stimulating factor gene. Nature 1990;345(6274):442-4
  • Campbell IK, Rich MJ, Bischof RJ, Hamilton JA. The colony-stimulating factors and collagen-induced arthritis: exacerbation of disease by M-CSF and G-CSF and requirement for endogenous M-CSF. J Leukoc Biol 2000;68(1):144-50
  • Isbel NM, Nikolic-Paterson DJ, Hill PA, Local macrophage proliferation correlates with increased renal M-CSF expression in human glomerulonephritis. Nephrol Dial Transplant 2001;16(8):1638-47
  • Yang PT, Xiao WG, Zhao LJ, Increase in the level of macrophage colony-stimulating factor in patients with systemic lupus erythematosus. Ann Rheum Dis 2008;67(3):429-30
  • Klebl FH, Olsen JE, Jain S, Doe WF. Expression of macrophage-colony stimulating factor in normal and inflammatory bowel disease intestine. J Pathol 2001;195(5):609-15
  • Rallidis LS, Zolindaki MG, Pentzeridis PC, Raised concentrations of macrophage colony stimulating factor in severe unstable angina beyond the acute phase are strongly predictive of long term outcome. Heart 2004;90(1):25-9
  • Kreipe H, Radzun HJ, Heidorn K, Proliferation, macrophage colony-stimulating factor, and macrophage colony-stimulating factor-receptor expression of alveolar macrophages in active sarcoidosis. Lab Invest 1990;62(6):697-703
  • Retamales I, Elliott WM, Meshi B, Amplification of inflammation in emphysema and its association with latent adenoviral infection. Am J Respir Crit Care Med 2001;164(3):469-73
  • Davis TA, Lennon G. Mice with a regenerative wound healing capacity and an SLE autoimmune phenotype contain elevated numbers of circulating and marrow-derived macrophage progenitor cells. Blood Cells Mol Dis 2005;34(1):17-25
  • Lenda DM, Kikawada E, Stanley ER, Kelley VR. Reduced macrophage recruitment, proliferation, and activation in colony-stimulating factor-1-deficient mice results in decreased tubular apoptosis during renal inflammation. J Immunol 2003;170(6):3254-62
  • Lenda DM, Stanley ER, Kelley VR. Negative role of colony-stimulating factor-1 in macrophage, T cell, and B cell mediated autoimmune disease in MRL-Fas(lpr) mice. J Immunol 2004;173(7):4744-54
  • Le Meur Y, Jose MD, Mu W, Macrophage colony-stimulating factor expression and macrophage accumulation in renal allograft rejection. Transplantation 2002;73(8):1318-24
  • Welsing PM, van Gestel AM, Swinkels HL, The relationship between disease activity, joint destruction, and functional capacity over the course of rheumatoid arthritis. Arthritis Rheum 2001;44(9):2009-17
  • Chu CQ, Field M, Allard S, Detection of cytokines at the cartilage/pannus junction in patients with rheumatoid arthritis: implications for the role of cytokines in cartilage destruction and repair. Br J Rheumatol 1992;31(10):653-61
  • Campbell IK, Ianches G, Hamilton JA. Production of macrophage colony-stimulating factor (M-CSF) by human articular cartilage and chondrocytes. Modulation by interleukin-1 and tumor necrosis factor [alpha]. Biochimica et Biophysica Acta (BBA) – Mol Basis Dis 1993;1182(1):57-63
  • Nakano K, Okada Y, Saito K, Rheumatoid synovial endothelial cells produce macrophage colony-stimulating factor leading to osteoclastogenesis in rheumatoid arthritis. Rheumatology (Oxford) 2007;46(4):597-603
  • Rioja I, Hughes FJ, Sharp CH, Potential novel biomarkers of disease activity in rheumatoid arthritis patients: CXCL13, CCL23, transforming growth factor alpha, tumor necrosis factor receptor superfamily member 9, and macrophage colony-stimulating factor. Arthritis Rheum 2008;58(8):2257-67
  • Komano Y, Nanki T, Hayashida K, Identification of a human peripheral blood monocyte subset that differentiates into osteoclasts. Arthritis Res Ther 2006;8(5):R152
  • Kitaura H, Zhou P, Kim H-J, M-CSF mediates TNF-induced inflammatory osteolysis. J Clin Investig 2005;115(12):3418-27
  • Menaa C, Barsony J, Reddy SV, 1,25-Dihydroxyvitamin D3 hypersensitivity of osteoclast precursors from patients with Paget's disease. J Bone Miner Res 2000;15(2):228-36
  • Neale SD, Smith R, Wass JA, Athanasou NA. Osteoclast differentiation from circulating mononuclear precursors in Paget's disease is hypersensitive to 1,25-dihydroxyvitamin D(3) and RANKL. Bone 2000;27(3):409-16
  • Menaa C, Reddy SV, Kurihara N, Enhanced RANK ligand expression and responsivity of bone marrow cells in Paget's disease of bone. J Clin Invest 2000;105(12):1833-8
  • Cody JD, Singer FR, Roodman GD, Genetic linkage of Paget disease of the bone to chromosome 18q. Am J Hum Genet 1997;61(5):1117-22
  • Laurin N, Brown JP, Lemainque A, Paget disease of bone: mapping of two loci at 5q35-qter and 5q31. Am J Hum Genet 2001;69(3):528-43
  • Haslam SI, Van Hul W, Morales-Piga A, Paget's disease of bone: evidence for a susceptibility locus on chromosome 18q and for genetic heterogeneity. J Bone Miner Res 1998;13(6):911-17
  • Roodman GD, Kurihara N, Ohsaki Y, Interleukin 6. A potential autocrine/paracrine factor in Paget's disease of bone. J Clin Invest 1992;89(1):46-52
  • Hoyland JA, Freemont AJ, Sharpe PT. Interleukin-6, IL-6 receptor, and IL-6 nuclear factor gene expression in Paget's disease. J Bone Miner Res 1994;9(1):75-80
  • Neale SD, Schulze E, Smith R, Athanasou NA. The influence of serum cytokines and growth factors on osteoclast formation in Paget's disease. QJM 2002;95(4):233-40
  • Rubin J, Fan X, Thornton D, Regulation of murine osteoblast macrophage colony-stimulating factor production by 1,25(OH)2D3. Calcif Tissue Int 1996;59(4):291-6
  • Gorer PA. Some recent work on tumor immunity. Adv Cancer Res 1956;4:149-86
  • Elgert KD, Alleva DG, Mullins DW. Tumor-induced immune dysfunction: the macrophage connection. J Leukoc Biol 1998;64(3):275-90
  • Lin EY, Li JF, Gnatovskiy L, Macrophages regulate the angiogenic switch in a mouse model of breast cancer. Cancer Res 2006;66(23):11238-46
  • Kacinski BM. CSF-1 and its receptor in ovarian, endometrial and breast cancer. Ann Med. 1995;27(1):79-85
  • Kacinski BM. CSF-1 and its receptor in breast carcinomas and neoplasms of the female reproductive tract. Mol Reprod Dev 1997;46(1):71-4
  • Xu FJ, Ramakrishnan S, Daly L, Increased serum levels of macrophage colony-stimulating factor in ovarian cancer. Am J Obstet Gynecol. 1991;165(5 Pt 1):1356-62
  • Mroczko B, Groblewska M, Wereszczynska-Siemiatkowska U, Serum macrophagecolony stimulating factor levels in colorectal cancer patients correlate with lymph node metastasis and poor prognosis. Clin Chim Acta 2007;380:208-12
  • Mroczko B, Szmitkowski M, Okulczyk B. Granulocyte-colony stimulating factor (G-CSF) and macrophage colony stimulating factor (M-CSF) in colorectal cancer patients. Clin Chem Lab Med 2002;40:351-5
  • Khatami M. Standardizing cancer biomarkers criteria: data elements as a foundation for a database. Inflammatory mediator/M-CSF as model marker. Cell Biochem Biophys 2007;47:187-98
  • Bingle L, Brown NJ, Lewis CE. The role of tumour-associated macrophages in tumour progression: implications for new anticancer therapies. J Pathol 2002;196(3):254-65
  • Pollard JW. Tumour-educated macrophages promote tumour progression and metastasis. Nat Rev Cancer 2004;4(1):71-8
  • Lewis CE, Pollard JW. Distinct role of macrophages in different tumor microenvironments. Cancer Res 2006;66(2):605-12
  • Aharinejad S, Paulus P, Sioud M, Colony-stimulating factor-1 blockade by antisense oligonucleotides and small interfering RNAs suppresses growth of human mammary tumor xenografts in mice. Cancer Res 2004;64(15):5378-84
  • Paulus P, Stanley ER, Schafer R, Colony-stimulating factor-1 antibody reverses chemoresistance in human MCF-7 breast cancer xenografts. Cancer Res 2006;66(8):4349-56
  • Kubota Y, Takubo K, Shimizu T, M-CSF inhibition selectively targets pathological angiogenesis and lymphangiogenesis. J Exp Med 2009;206(5):1089-102
  • Manthey CL, Johnson DL, Illig CR, JNJ-28312141, a novel orally active colony-stimulating factor-1 receptor/FMS-related receptor tyrosine kinase-3 receptor tyrosine kinase inhibitor with potential utility in solid tumors, bone metastases, and acute myeloid leukemia. Mol Cancer Ther 2009;8(11):3151-61
  • Biswas SK, Gangi L, Paul S, A distinct and unique transcriptional program expressed by tumor-associated macrophages (defective NF-kappaB and enhanced IRF-3/STAT1 activation). Blood 2006;107:2112-22
  • Saccani A, Schioppa T, Porta C, p50 nuclear factor-kappaB overexpression in tumor-associated macrophages inhibits M1 inflammatory responses and antitumor resistance. Cancer Res 2006;66:11432-40
  • Coussens LM, Werb Z. Inflamm Cancer Nat 2002;420:860-67
  • Lewis CE, Pollard JW. Distinct role of macrophages in different tumor microenvironments. Cancer Res 2006;66:605-12
  • Nowicki A, Szenajch J, Ostrowska G, Impaired tumor growth in colony-stimulating factor 1 (CSF-1)-deficient, macrophage-deficient op/op mouse: evidence for a role of CSF-1-dependent macrophages in formation of tumor stroma. Int J Cancer 1996;65(1):112-19
  • Patel S, Player MR. Colony-stimulating factor-1 receptor inhibitors for the treatment of cancer and inflammatory disease. Curr Top Med Chem 2009;9:599-610
  • AstraZeneca Ltd. Chemical Compounds. WO2006067445; 2006
  • AstraZeneca Ltd. Chemical Compounds. WO2007071955; 2007
  • Scott DA, Aquila BM, Bebernitz GA, Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer. Bioorg Med Chem Lett 2008;18(17):4794-7
  • 3 Dimensional Pharmaceuticals, Inc. c-FMS kinase inhibitors WO2004096795; 2004
  • Janssen Pharmaceutica N.V. Inhibitors of c-fms kinase. WO2006047503; 2006
  • Janssen Pharmaceutica N.V. Inhibitors of c-FMS kinase. WO2006047277; 2006
  • Janssen Pharmaceutica N.V. Aromatic amides as inhibitors of c-FMS kinase. WO2006047504; 2006
  • Janssen Pharmaceutica N.V. Inhibitors of c-FMS kinase. WO2007124322; 2007
  • Janssen Pharmaceutica N.V. c-fms kinase inhibitors. WO2007123516; 2007
  • Janssen Pharmaceutica N.V. Use of cfms inhibitor for treating or preventing bone cancer and the bone loss and bone pain associated with bone cancer. WO2009058801; 2009
  • Patch RJ, Brandt BM, Asgari D, Potent 2′-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents. Bioorg Med Chem Lett 2007;17(22):6070-4
  • Illig CR, Chen J, Wall MJ, Discovery of novel FMS kinase inhibitors as anti-inflammatory agents. Bioorg Med Chem Lett 2008;18(5):1642-8
  • Meegalla SK, Wall MJ, Chen J, Structure-based optimization of a potent class of arylamide FMS inhibitors. Bioorg Med Chem Lett 2008;18(12):3632-7
  • GlaxoSmithKline. Crystal Structure of liganded cFMS kinase domain. US20040002145; 2004
  • Conway JG, McDonald B, Parham J, Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580. Proc Natl Acad Sci USA 2005;102(44):16078-83
  • Conway JG, Pink H, Bergquist ML, Effects of the cFMS Kinase Inhibitor 5-(3-Methoxy-4-((4-methoxybenzyl)oxy)benzyl)pyrimidine-2,4-diamine (GW2580) in Normal and Arthritic Rats. J Pharmacol Exp Ther 2008;326(1):41-50
  • Pfizer, Inc. Pyrazole-substituted aminoheteroaryl compounds as protein kinase inhibitors. WO2006021881; 2006
  • Cytopia Research Pty Ltd. Inhibitors of Kinase Activity. WO2008058341; 2008
  • Burns CJ, Harte MF, Bu X, Discovery of 2-([alpha]-methylbenzylamino) pyrazines as potent Type II inhibitors of FMS. Bioorg Med Chem Lett 2009;19(4):1206-9
  • Kirin Brewery. Quinoline derivatives and quinazoline derivatives inhibiting autophosphorylation of macrophage colony stimulating factor receptor. WO200309328; English version EP1535910; 2003
  • Ohno H, Kubo K, Murooka H, A c-fms tyrosine kinase inhibitor, Ki20227, suppresses osteoclast differentiation and osteolytic bone destruction in a bone metastasis model. Mol Cancer Ther 2006;5(11):2634-43
  • Ohno H, Uemura Y, Murooka H, The orally-active and selective c-Fms tyrosine kinase inhibitor Ki20227 inhibits disease progression in a collagen-induced arthritis mouse model. Eur J Immunol 2008;38(1):283-91
  • Uemura Y, Ohno H, Ohzeki Y, The selective M-CSF receptor tyrosine kinase inhibitor Ki20227 suppresses experimental autoimmune encephalomyelitis. J Neuroimmunol 2008;195(1-2):73-80
  • Kubota Y, Takubo K, Shimizu T, M-CSF inhibition selectively targets pathological angiogenesis and lymphangiogenesis. J Exp Med 2009;206(5):1089-102
  • Smalley Jr TL, Chamberlain SD, Mills WY, Synthesis of novel anilinoquinolines as c-fms inhibitors. Bioorg Med Chem Lett 2007;17(22):6257-60
  • AstraZeneca Ltd. 4-Anilinoquinoline-3-Carboxamides As CSF-1R Kinase Inhibitors. WO2007119046; 2007
  • AstraZeneca Ltd. Chemical Compounds. WO2008056148; 2008
  • Scott DA, Balliet CL, Cook DJ, Identification of 3-amido-4-anilinoquinolines as potent and selective inhibitors of CSF-1R kinase. Bioorg Med Chem Lett 2009;19(3):697-700
  • Scott DA, Bell KJ, Campbell CT, 3-Amido-4-anilinoquinolines as CSF-1R kinase inhibitors 2: optimization of the PK profile. Bioorg Med Chem Lett 2009;19(3):701-5
  • Drew L, Bell K, Dakin L, The selective CSF-1R inhibitor AZ683 reduces tumor associated macrophages and inhibits growth of breast cancer xenograft models (Abstract nr 259). In: Proceedings of the 100th Annual Meeting of the American Association for Cancer Research; 18 – 22 April 2009; Denver, CO. Philadelphia, PA, AACR; 2009
  • Plexxikon, Inc. Compounds modulating c-kit and c-fms activity and uses therefor. WO2007013896; 2007
  • Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor. WO2008080015; 2008
  • Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor. WO2008063888; 2008
  • Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor. WO2008064265; 2008
  • Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor. WO2009143018; 2009
  • Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor. US20090306086; 2009
  • Guo J, Marcotte PA, McCall JO, Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors. Mol Cancer Ther 2006;5(4):1007-13
  • West BL, DeNardo DG, Tsai J, Efficacy of the selective CSF-1R kinase inhibitor PLX3397 in mouse models of tumor growth and bone metastasis. (Abstract nr 3850). In: Proceedings of the 101st Annual Meeting of the American Association for Cancer Research; 17 – 21 April 2010; Washington, DC. Philadelphia, PA, AACR; 2010
  • Plexxikon's PLX3397 Preclinical Data Demonstrate Potential of Novel, “First-in-Class” Cancer Drug. Plexxikon, Inc. press release; 2010. Available from: www.plexxikon.com/view.cfm/73/Press-Releases [Last accessed 8 August 2010]
  • El-Gamal MI, Jung MH, Oh CH. Discovery of a new potent bisamide FMS kinase inhibitor. Bioorg Med Chem Lett 2010;20(11):3216-18
  • Korea Institute of Science and Technology. Novel pyrrolo[3,2-b]pyridine derivatives or pharmaceutically acceptable salt thereof, preparation method thereof and pharmaceutical composition for prevention or treatment of melanoma containing the same as an active ingredient. KR20100047998; 2010
  • Janssen Pharmaceutica N.V. Quinolinone derivatives as inhibitors of c-fms kinase WO2005009967; 2005
  • Wall MJ, Chen J, Meegalla S, Synthesis and evaluation of novel 3,4,6-substituted 2-quinolones as FMS kinase inhibitors. Bioorg Med Chem Lett 2008;18(6):2097-102
  • Janssen Pharmaceutica N.V. 5-Oxo-5,8-dihydro-pyrido-pyrimidines as inhibitors of c-FMS kinase. WO2007033137; 2007
  • Janssen Pharmaceutica N.V. 5-Oxo-5,8-dihydro-pyrido-pyrimidines as inhibitors of c-FMS kinase. WO2007033232; 2007
  • Janssen Pharmaceutica N.V. 5-Oxo-5,8-dihydro-pyrido-pyrimidines as inhibitors of c-FMS kinase. WO2008055013
  • Novartis AG. 6-O-Substituted benzoxazole and benzothiazole compounds and methods of inhibiting CSF1R signalling. WO2007121484; 2007
  • Novartis AG. 2 CSF-1R inhibitors, compositions, and methods of use. WO200814406; 2008
  • Novartis AG. 2 CSF-1R inhibitors, compositions, and methods of use. WO2009050228; 2009
  • Wiesmann M, Daniel DL, Pryer N, BLZ945, a selective c-fms (CSF-1R) kinase inhibitor for the suppression of tumor-induced osteolytic lesions in bone (Abstract nr 3629). In: Proceedings of the 101st Annual Meeting of the American Association for Cancer Research; 17 –21 April 2010; Washington, DC. Philadelphia, PA, AACR; 2010
  • Fedorov O, Muller S, Knapp S. The (un)targeted cancer kinome. Nat Chem Biol 2010;6(3):166-9
  • Buchdunger E, Cioffi CL, Law N, Abl protein-tyrosine kinase inhibitor STI571 inhibits in vitro signal transduction mediated by c-kit and platelet-derived growth factor receptors. J Pharmacol Exp Ther 2000;295(1):139-45
  • Dewar AL, Cambareri AC, Zannettino AC, Macrophage colony-stimulating factor receptor c-fms is a novel target of imatinib. Blood 2005;105(8):3127-32
  • Liu Y, Gray NS. Rational design of inhibitors that bind to inactive kinase conformations. Nat Chem Biol 2006;2(7):358-64
  • Swinney DC. Biochemical mechanisms of drug action: what does it take for success? Nat Rev Drug Discov 2004;3(9):801-8

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.